N-{[1-(2-phenylethyl)pyrrolidin-2-yl]methyl}cyclohexane-carboxamides as selective 5-HT1A receptor agonists

Authors
Fujio, M Togo, Y Tomozane, H Kuroita, T Morio, Y Katayama, J Matsumoto, Y
Citation
M. Fujio et al., N-{[1-(2-phenylethyl)pyrrolidin-2-yl]methyl}cyclohexane-carboxamides as selective 5-HT1A receptor agonists, BIOORG MED, 10(5), 2000, pp. 509-512
Citations number
16
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
5
Year of publication
2000
Pages
509 - 512
Database
ISI
SICI code
0960-894X(20000306)10:5<509:NAS>2.0.ZU;2-U
Abstract
A series of benzamides was synthesized as selective agonists for the 5-HT1A receptor. It was found that (S)-N-{[1-(2-phenylethyl)pyrrolidin-2-yl]methy l}cyclohexanecarboxamide(7-(S)) has potent and selective agonistic activity for the 5-HT1A receptor (5-HT1A; K-i = 0.49 nmol/L, D-2; IC50 = >1000 nmol /L, 5-HT2; K-i = 240 nmol/L). (C) 2000 Elsevier Science Ltd. All rights res erved.